用高效液相色谱法研究阿糖胞苷在家兔中的药代动力学

PHARMACOKINETIC STUDY OF Ara-C IN THE RABBIT BY HIGH PERFORMANCE LIQUID CHROMATOGRAPHY

我们建立用高效液相色谱法(HPLC)测定血浆中阿糖胞苷(Ara-C)浓度的方法。Ara-C血浆浓度在1～10μg/ml范围内为直线相关,r=0.9994。方法回收率为96.67％。最低检测限为5ng;血浆中最低检测浓度为200ng/ml。5只家兔,每只静脉注射Ara-C 5mg-剂量,用本文的HPLC方法测定其血浆浓度,所得药代动力学参数平均值为:K=0.7611 h^(-1),t_(1/2)=0.9324h,Vd=2.935L/kg,Cl=2.246L/(h·kg)。其结果符合单室模型,对本法的优点作了讨论。

A method to estimate plasma levels of 1-β-D-arabinofuranosylcytosine (Ara-C) using high performance liquid chromatography (PHLC) was established. The calibration curve was linear for concentrations from 1-10μg/ml plasma, r = 0.999 4. The recovery was 96.67%. The limit of detection was 5ng, and its detectable plasma concentration was 200ng/ml.Each of 5 rabbits was given an .intravenous dose of 5mg Ara-C. The plasma concentrations were determined by this HPLC method. The mean pharmaookinetic parameters of Ara-C obtained were as follows: K=0.7611h-1, t1/2=0.932 4h Vd = 2.935L/kg,Cl=2.246L/(h·kg). Besults fit a one-compartment model. The advantages of this method are discussed.